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PE20011314A1 - DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA - Google Patents

DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA

Info

Publication number
PE20011314A1
PE20011314A1 PE2001000442A PE2001000442A PE20011314A1 PE 20011314 A1 PE20011314 A1 PE 20011314A1 PE 2001000442 A PE2001000442 A PE 2001000442A PE 2001000442 A PE2001000442 A PE 2001000442A PE 20011314 A1 PE20011314 A1 PE 20011314A1
Authority
PE
Peru
Prior art keywords
phenyl
carbamimidoyl
glycin
derivatives
ixa
Prior art date
Application number
PE2001000442A
Other languages
English (en)
Inventor
Leo Alig
Kurt Hilpert
Katrin Groebke Zbinden
Ulrike Obst
Hans Peter Wessel
Holger Kuehne
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20011314A1 publication Critical patent/PE20011314A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D317/34—Oxygen atoms
    • C07D317/36—Alkylene carbonates; Substituted alkylene carbonates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
    • C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/20—Oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA DE FORMULA I DONDE R1 ES ALQUILO; R2 ES H, HIDROXIALCOXILO, ALCOXICARBONILOXI, ALCOXILO, ENTRE OTROS; R3 ES H, ALCOXILO, HETEROCICLOALQUILOXILO; R4 ES H, ESTER; R5 ES H, HIDROXILO, ALCOXICARBONILO, HALOGENOALCOXICARBONILO, ENTRE OTROS; X ES F, Cl, Br. SON COMPUESTOS PREFERIDOS ESTER ETILICO DEL ACIDO (RS)-(4-CARBAMIMIDOIL-FENILAMINO)-3,5-DIETOXI-2-FLUORO-FENIL-ACETICO, ACIDO (RS)-(4-CARBAMIMIDOIL-FENILAMINO)-(2-FLUORO-3,5-DIMETOXI-FENIL)-ACETICO, ESTER ETILICO DEL ACIDO (RS)-(4-CARBAMIMIDOIL-FENILAMINO)-(2-FLUORO-3,5-DIMETOXI-FENIL)-ACETICO. LOS DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA SON INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA Y SON UTILES PARA LA PREVENCION Y TRATAMIENTO DE TROMBOSIS, APOPLEJIA, INFARTO CARDIACO
PE2001000442A 2000-05-23 2001-05-17 DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA PE20011314A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00110881 2000-05-23

Publications (1)

Publication Number Publication Date
PE20011314A1 true PE20011314A1 (es) 2002-01-04

Family

ID=8168800

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001000442A PE20011314A1 (es) 2000-05-23 2001-05-17 DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA

Country Status (23)

Country Link
US (1) US6548694B2 (es)
EP (1) EP1289939A1 (es)
JP (1) JP3842132B2 (es)
KR (1) KR100569517B1 (es)
CN (1) CN1305839C (es)
AR (1) AR028596A1 (es)
AU (2) AU2001281774B2 (es)
BR (1) BR0110998A (es)
CA (1) CA2408602C (es)
EC (1) ECSP024360A (es)
HU (1) HUP0302073A2 (es)
IL (1) IL152581A0 (es)
MA (1) MA26905A1 (es)
MX (1) MXPA02011466A (es)
NO (1) NO20025590L (es)
NZ (1) NZ522412A (es)
PE (1) PE20011314A1 (es)
PL (1) PL361355A1 (es)
RU (1) RU2268257C2 (es)
UY (1) UY26721A1 (es)
WO (1) WO2001090051A1 (es)
YU (1) YU83602A (es)
ZA (1) ZA200208899B (es)

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HK1043106A1 (zh) * 1998-12-14 2002-09-06 F. Hoffmann-La Roche Ag 苯基甘氨酸衍生物
DE10300049A1 (de) * 2003-01-03 2004-07-15 Morphochem AG Aktiengesellschaft für kombinatorische Chemie Neue Verbindungen, die Faktor VIIa inhibieren
US6642386B2 (en) * 2002-02-06 2003-11-04 Hoffmann-La Roche Inc. N-(4-carbamimidoyl-phenyl)-glycine derivatives
GB0211931D0 (en) * 2002-05-23 2002-07-03 Univ Liverpool Methods & device utilizing adsorption of molecules at a surface or interface
TW200410921A (en) * 2002-11-25 2004-07-01 Hoffmann La Roche Mandelic acid derivatives
EP1594505A4 (en) 2003-02-11 2008-08-13 Bristol Myers Squibb Co PHENYLGLYCIN DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS
WO2004072102A2 (en) 2003-02-11 2004-08-26 Bristol-Myers Squibb Company Benzene acetamide compounds useful as serine protease inhibitors
DE10306202A1 (de) 2003-02-13 2004-08-26 Grünenthal GmbH Arzneimittel enthaltend substituierte 2-Aryl-Aminoessigsäure-Verbindungen und/oder substituierte 2-Heteroaryl-Aminoessigsäure-Verbindungen
US7917130B1 (en) 2003-03-21 2011-03-29 Stratosaudio, Inc. Broadcast response method and system
US7776804B2 (en) * 2005-03-16 2010-08-17 The Lubrizol Corporation Viscosity improver compositions providing improved low temperature characteristics to lubricating oil
US7056932B2 (en) * 2003-12-19 2006-06-06 Hoffman-La Roche Inc. Heterocyclyl substituted 1-alkoxy acetic acid amides
WO2006041119A1 (ja) * 2004-10-13 2006-04-20 Eisai R & D Management Co., Ltd. ヒドラジド誘導体
EP1838296B1 (en) * 2004-10-20 2012-08-08 Resverlogix Corp. Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
WO2006076246A2 (en) 2005-01-10 2006-07-20 Bristol-Myers Squibb Company Phenylglycinamide derivatives useful as anticoagulants
ATE455103T1 (de) * 2005-06-24 2010-01-15 Bristol Myers Squibb Co Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate
EP1996541B1 (en) * 2006-03-09 2014-04-23 Bristol-Myers Squibb Company 2-(aryloxy)acetamide factor viia inhibitors useful as anticoagulants
MX2008012031A (es) * 2006-03-24 2008-10-02 Eisai R&D Man Co Ltd Derivado de triazolona.
US7855194B2 (en) 2006-03-27 2010-12-21 Hoffmann-La Roche Inc. Pyrimidine, quinazoline, pteridine and triazine derivatives
AU2007345526B2 (en) 2007-02-01 2013-02-28 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular diseases
EP1967522A1 (en) * 2007-03-07 2008-09-10 Novo Nordisk A/S New blood coagulation factor inhibitors
JPWO2009038157A1 (ja) * 2007-09-21 2011-01-06 エーザイ・アール・アンド・ディー・マネジメント株式会社 ２，３−ジヒドロ−イミノイソインドール誘導体
WO2009079417A1 (en) 2007-12-14 2009-06-25 Stratosaudio, Inc. Systems and methods for scheduling interactive media and events
WO2009158404A1 (en) * 2008-06-26 2009-12-30 Resverlogix Corp. Methods of preparing quinazolinone derivatives
NZ594332A (en) 2009-01-08 2013-09-27 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular disease
KR101709492B1 (ko) 2009-03-18 2017-02-23 리스버로직스 코퍼레이션 신규한 소염제
ES2706651T3 (es) 2009-04-22 2019-03-29 Resverlogix Corp Nuevos agentes antiinflamatorios
CN102887836B (zh) * 2011-07-18 2014-03-26 西南大学 L-苯甘氨酸衍生物及其应用
SI2773354T1 (sl) 2011-11-01 2019-08-30 Resverlogix Corp. Peroralne formulacije s takojšnjim sproščanjem za substituirane kinazolinone
GB201118876D0 (en) * 2011-11-01 2011-12-14 Astex Therapeutics Ltd Pharmaceutical compounds
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
KR20150096794A (ko) 2012-12-21 2015-08-25 제니쓰 에피제네틱스 코포레이션 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물
KR102662814B1 (ko) 2015-03-13 2024-05-03 리스버로직스 코퍼레이션 보체 관련 질환을 치료하기 위한 조성물 및 치료 방법
CN111072562B (zh) * 2019-11-07 2021-12-07 中山大学 一种四氢异喹啉衍生物及其制备方法和应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
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CA2008116C (en) * 1989-02-23 2001-11-20 Thomas Weller Glycine derivatives
DE4421052A1 (de) * 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
DE59808751D1 (de) 1997-12-04 2003-07-24 Hoffmann La Roche N-(4-carbamimido-phenyl)-glycinamidderivate
US6358960B1 (en) * 1998-02-17 2002-03-19 Ono Pharmaceutical Co., Ltd. Amidino derivatives and drugs containing the same as the active ingredient
HK1043106A1 (zh) * 1998-12-14 2002-09-06 F. Hoffmann-La Roche Ag 苯基甘氨酸衍生物

Also Published As

Publication number Publication date
US6548694B2 (en) 2003-04-15
JP3842132B2 (ja) 2006-11-08
ZA200208899B (en) 2004-02-19
JP2003534311A (ja) 2003-11-18
KR20030007678A (ko) 2003-01-23
CA2408602C (en) 2008-01-08
HUP0302073A2 (hu) 2003-09-29
KR100569517B1 (ko) 2006-04-07
IL152581A0 (en) 2003-05-29
AU2001281774B2 (en) 2005-03-10
CN1430599A (zh) 2003-07-16
NO20025590D0 (no) 2002-11-21
PL361355A1 (en) 2004-10-04
AR028596A1 (es) 2003-05-14
NZ522412A (en) 2004-05-28
EP1289939A1 (en) 2003-03-12
MXPA02011466A (es) 2003-04-25
UY26721A1 (es) 2001-12-28
US20020004608A1 (en) 2002-01-10
CN1305839C (zh) 2007-03-21
AU8177401A (en) 2001-12-03
WO2001090051A1 (en) 2001-11-29
RU2268257C2 (ru) 2006-01-20
NO20025590L (no) 2002-11-21
YU83602A (sh) 2006-05-25
CA2408602A1 (en) 2001-11-29
ECSP024360A (es) 2003-03-31
BR0110998A (pt) 2003-04-08
MA26905A1 (fr) 2004-12-20

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